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41. 发明公开

EP1790640A4 NOVEL IMIDAZOLIDINE DERIVATIVE AND USE THEREOF 审中-公开
标题翻译：新咪唑及其用途
公开(公告)号：EP1790640A4
公开(公告)日：2009-07-29
申请号：EP05782020
申请日：2005-09-09
申请人： CHUGAI PHARMACEUTICAL CO LTD
发明人： TACHIBANA KAZUTAKA , SATO HARUHIKO , OHTA MASATERU , NAKAMURA MITSUAKI , SHIRAISHI TAKUYA , YOSHINO HITOSHI , EMURA TAKASHI , HONMA AKIE , ONUMA ETSURO , KAWATA HIROMITSU , TANIGUCHI KENJI
IPC分类号： C07D233/86 , A61K31/4166 , A61K31/428 , A61K31/454 , A61K31/496 , A61P5/24 , A61P5/28 , A61P13/08 , A61P17/00 , A61P17/08 , A61P17/10 , C07D211/58 , C07D233/74
CPC分类号： C07D417/04 , C07D211/58 , C07D233/74 , C07D233/86 , C07D277/82 , C07D401/04
摘要： A compound represented by the formula (I): [Chemical formula 1] (I) [wherein Q is a group represented by the formula; [Chemical formula 2] (X) or (Y) A is hydrogen, halogeno, -ORa, or C1-4 alkyl optionally substituted by one or more halogen atoms; E's each independently is C1-6 alkyl; m is an integer of 0-3; R2 and R3 each independently is C1-6 alkyl; X1 and X2 each independently is O or S; Y is one member selected among arylene, a divalent 5- or 6-membered monocyclic heterocyclic group, and a divalent 8- to 10-membered fused-ring heterocyclic group;and Z is -CON(-Ra)-, -CO-, -COO-, -NRa-C(=NH)NRb-, -NRa-(C=N-CN)NRb-, -N(-Ra)COO-, -C(=NH)-, -SO2-, -SO2N(-Ra)-, -SO2NR1-, -N(-Ra)CO-, -N(-Ra)CON(-Rb)-, -N(COR1)CO-, -N(-Ra)SO2-, -N(SO2R1)SO2-, -N(-Ra)-, or -N(-Ra)SO2N(-Rb)-], or a salt, prodrug, or solvate of the compound. Also provided is a medicinal composition containing the compound or the like.

42. 发明公开

EP0702952A4 BENZOPYRAN DERIVATIVE 失效
标题翻译：苯并吡喃
公开(公告)号：EP0702952A4
公开(公告)日：1996-02-02
申请号：EP94913810
申请日：1994-04-25
申请人： CHUGAI PHARMACEUTICAL CO LTD
发明人： KOGA HIROSHI , SATO HARUHIKO , ISHIZAWA TAKENORI
IPC分类号： C07D311/58 , A61K31/35
CPC分类号： C07D311/58
摘要： A benzopyran derivative represented by general formula (I) and a pharmaceutically acceptable salt thereof, whrein R, X and Y represent together any of the combinations represented by (A). These compounds are excellent in the potassium channel activity and also in safety.

43. 发明公开

EP0205872A1 Furobenzisoxazole derivatives. 失效
标题翻译： Furobenzisoxazolderivate。
公开(公告)号：EP0205872A1
公开(公告)日：1986-12-30
申请号：EP86106437
申请日：1986-05-12
申请人： CHUGAI PHARMACEUTICAL CO LTD
发明人： SATO HARUHIKO , KOGA HIROSHI , DAN TAKASHI , ONUMA ETSURO
IPC分类号： C07D498/04 , A61K31/42
CPC分类号： C07D498/04
摘要： Novel furobenzisoxazole derivatives of the formule (I):

(wherein R
1 , R
2 , R
3 and R
4 which may be the same or different represent a hydrogen atom, a halogen atom, or a lower alkyl group having 1-4 carbon atoms; R
5 is a hydroxymethyl group, a carboxyl group or a lower alkoxy carbonyl group having 1-3 carbon atoms; and X is a sulfur atom or a-CH =CH-group), as well as intoxic salts thereof when R, is a carboxyl group, and process for preparing the same are disclosed.
The drivatives of formula (I) and intoxic salts thereof have hypotensive, uricosuric and diuretic activities and hence are useful as therapeutics for treating hyperuricemia, edema and hypertension.
摘要翻译：式（I）的新型呋喃苯并异恶唑衍生物:(其中R 1，R 2，R 3和R 4可以相同或不同，表示氢原子，卤素原子或具有1-4个碳原子的低级烷基 ; R 5是羟基甲基，羧基或具有1-3个碳原子的低级烷氧基羰基; X是硫原子或-CH = CH-基团），以及当R 1是羧基及其制备方法。式（I）的驱虫剂和其不含毒性的盐具有降血压，促尿酸尿和利尿作用，因此可用作治疗高尿酸血症，水肿和高血压的治疗剂。

44. 发明公开

EP2045253A4 alpha-AMINO ACID DERIVATIVE AND PHARMACEUTICAL COMPRISING THE SAME AS ACTIVE INGREDIENT 审中-公开
标题翻译： α-氨基酸衍生物和药物，这作为活性成分的
公开(公告)号：EP2045253A4
公开(公告)日：2013-01-23
申请号：EP07767879
申请日：2007-06-29
申请人： NISSAN CHEMICAL IND LTD , CHUGAI PHARMACEUTICAL CO LTD
发明人： OHRAI KAZUHIKO , ADACHI MICHIAKI , TOYAMA KOJI , SHIMIZU TAKANORI , HAYASHI KEISHI , MINAMI MASATAKA , SUZUKI YOSHIYUKI , SUGIYAMA MASAKAZU , OHTA MASATERU , KADONO SHOJIRO , SHIRAISHI TAKUYA , SATO HARUHIKO , WATANABE YOSHIAKI , ISHII NOBUYA , SAKAITANI MASAHIRO , HASEGAWA MASAMI
IPC分类号： C07D513/04 , A61K31/429 , A61K31/4439 , A61P9/04 , A61P35/00 , A61P43/00
CPC分类号： C07D513/04

45. 发明公开

EP1724287A4 HYALURONIC ACID/METHOTREXATE COMPOUND 审中-公开
标题翻译：透明质酸/甲氨蝶呤CONNECTION
公开(公告)号：EP1724287A4
公开(公告)日：2010-10-27
申请号：EP05720011
申请日：2005-03-04
申请人： DENKI KAGAKU KOGYO KK , CHUGAI PHARMACEUTICAL CO LTD
发明人： IKEYA HITOSHI , MORIKAWA TADASHI , TAKAHASHI KOICHI , TAMURA TATSUYA , OKAMACHI AKIRA , ISHIZAWA TAKENORI , SATO HARUHIKO , HIGUCHI YOSHINOBU
IPC分类号： C08B37/08 , A61K31/519 , A61K47/48 , A61P19/02 , C07D475/10 , C07K5/00 , C07K9/00
CPC分类号： C08B37/0072 , A61K47/61 , A61K47/65 , C07D475/08 , C07K9/003
摘要： An object of the present invention is to provide a hyaluronic acid-methotrexate conjugate useful as a therapeutic drug for joint diseases. There is provided a hyaluronic acid-methotrexate conjugate useful as a therapeutic drug for joint diseases, wherein methotrexate is conjugated with a carboxyl group of hyaluronic acid through a linker containing a peptide chain consisting of 1 to 8 amino acids.

46. 发明公开

EP1775289A4 NOVEL IMIDAZOLIDINE DERIVATIVES 有权
标题翻译：新咪唑
公开(公告)号：EP1775289A4
公开(公告)日：2009-09-02
申请号：EP05768418
申请日：2005-08-03
申请人： CHUGAI PHARMACEUTICAL CO LTD
发明人： TACHIBANA KAZUTAKA , SATO HARUHIKO , OHTA MASATERU , NAKAMURA MITSUAKI , SHIRAISHI TAKUYA , IMAOKA IKUHIRO , YOSHINO HITOSHI , NAGAMUTA MASAHIRO , KAWATA HIROMITSU
IPC分类号： C07D233/66 , A61K31/4164 , A61P13/08 , A61P15/00 , A61P17/00 , A61P17/08 , A61P17/14 , A61P35/00 , A61P43/00
CPC分类号： C07D233/86 , C07D233/76
摘要： Compounds represented by the general formula (I); and drugs and medicinal compositions, containing the compounds: (I) wherein n is an integer of 1 to 20; Q is (II) or (III) A is cyano or the like; B is hydrogen, halogeno, or the like; X1 and X2 are each independently selected from between O and S; E is C1-4 alkyl; and R1, R2, R3 and R4 are each independently selected from between hydrogen and C1-6 alkyl.

47. 发明公开

EP1364960A4 PEPTIDE DERIVATIVES 审中-公开
标题翻译：肽衍生物
公开(公告)号：EP1364960A4
公开(公告)日：2005-05-18
申请号：EP02711294
申请日：2002-02-04
申请人： CHUGAI PHARMACEUTICAL CO LTD
发明人： SHIRAISHI TAKUYA , KADONO SHOJIRO , HARAMURA MASAYUKI , SATO HARUHIKO , KOZONO TOSHIRO , KOGA TAKAKI , SAKAMOTO AKIHISA
IPC分类号： A61K38/00 , C07K5/06 , C07K5/065 , C07K5/078 , G01N33/68 , C07K5/062 , C07K14/745 , G01N33/15 , G06F17/50
CPC分类号： G06F19/16 , A61K38/00 , C07K5/06078 , C07K5/06139 , C07K5/06156 , G01N33/68
摘要： Compounds represented by the following general formula (1): (1) wherein R1 represents amidinophenyl, etc.; R2 represents hydrogen, etc.; R3 represents carbamoylalkyl, etc.; R4 represents hydrogen, etc.; R5 represents benzyl, etc.; R6 represents hydrogen, etc.; and R7 represents alkylsulfonyl, etc. Crystals of a complex of VIIa factor/human soluble tissue factor with a low-molecular weight reversible VIIa factor inhibitor. A medium carrying the whole or a part of the coordinate data of the stereostructure of the complex of human VIIa factor/human soluble tissue factor with a low-molecular weight reversible VIIa factor inhibitor obtained by X-ray crystal structure analysis of the above crystals recorded thereon. A method of designing a low-molecular weight reversible VIIa factor inhibitor by using the above data.

48. 发明专利

JPH09227537A SYDNONE IMINE DERIVATIVE 失效
公开(公告)号：JPH09227537A
公开(公告)日：1997-09-02
申请号：JP32751496
申请日：1996-11-01
申请人： CHUGAI PHARMACEUTICAL CO LTD
发明人： KOGA HIROSHI , SATO HARUHIKO , TAKAHASHI TADAKATSU , IMAGAWA JUNICHI
IPC分类号： C07D271/04 , A61K31/435 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5377 , A61K31/54 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , C07D413/04 , C07D413/12 , C07D417/12
摘要： PROBLEM TO BE SOLVED: To obtain a new sydnone imine derivative having excellent vasodilator action, platelet aggregation-suppressing action, cardiac muscle protecting action and useful as a medicine. SOLUTION: This compound is represented by formula I Z is A-X-R1 [A is an alkylene; X is S(O)n [(n) is 0-2] or direct bond; R1 is an aryl, an arylcarbonyl, an alkyl, etc.]; R2 is N(R3 )R4 (R3 is H, an alkyl; R4 is H, an alkyl, an alkenyl, an alkynyl, an aryl, cycloalkyl, etc.), a group of formula II [R5 and R6 are each H or an alkyl; Y is O, S(O)n, etc.], etc.} or its salt which is permisible as a medicine, e.g. N [(3,5-di-t-butyl-4-hydroxyphenylthio) acetyl]-3-(4-methylpiperazine-1-yl)sydnoneimine. The compound of formula I is obtained by acylating a compound of formula III [(n) is 1 or 2].

49. 发明专利

JPH07316050A URICOTELIC AGENT CONTAINING OPTICALLY ACTIVE FUROBENZISOXAZOLE DERIVATIVE AS ACTIVE INGREDIENT 失效
公开(公告)号：JPH07316050A
公开(公告)日：1995-12-05
申请号：JP5107592
申请日：1992-01-24
申请人： CHUGAI PHARMACEUTICAL CO LTD
发明人： SATO HARUHIKO , DAN TAKASHI , KONUMA ETSURO , TANAKA HARUKO , AOKI BUNYA , KOGA HIROSHI
IPC分类号： C07D498/04 , A61K31/42 , A61P19/06 , C07B57/00
摘要： PURPOSE:To obtain an optically active uricotelic agent containing a furobenzisoxazole derivative which is the S(-)-isomer as an active ingredient. CONSTITUTION:This uricotelic agent contains S(-)-5-chloro-7,8-dihydro-3-pheny1 furo[2,3-g]-1,2-benzisoxazole-7-carboxylic acid expressed by formula I as an active ingredient. The compound expressed by formula I is obtained by dissolving a racemic modification expressed by formula II in an organic solvent, separating one optical isomer that is the R(+)-isomer with a basic optical resolving agent comprising preferably (-)-cinchonidine, then recovering a carboxylic acid substance from the mother liquor, adding a basic optical resolving agent preferably comprising (+)-phenylethylamine, etc., to the recovered carboxylic acid substance, depositing a crystal, repeating the recrystallization, purifying the resultant crystal, subsequently acidifying the crystal, removing bases and further repeating the recrystallization.

50. 发明专利

JPH07215986A NITRO COMPOUND 失效
公开(公告)号：JPH07215986A
公开(公告)日：1995-08-15
申请号：JP33372394
申请日：1994-12-06
申请人： CHUGAI PHARMACEUTICAL CO LTD
发明人： KOGA HIROSHI , SATO HARUHIKO , TAKAHASHI TADAKATSU
IPC分类号： A61K31/66 , A61P9/08 , A61P9/10 , C07F9/38 , C07F9/40 , C07F9/44
摘要： PURPOSE:To obtain a new nitro compound, comprising 1-hydroxyimino-4-nitro-2- alkenylphosphoric acid diesters, having strong vasodilator actions and useful as an orally administrable therapeutic agent, etc., for angina pectoris. CONSTITUTION:This new nitro compound is expressed by formula I [R1 and R2 each is H, a (substituted) lower alkyl or an (substituted) aromatic hydrocarbon; R3 is H, a (substituted) lower alkyl or an (substituted) aromatic hydrocarbon or R1 (or R2), together with R3, denotes an (substituted) aklylene; R4 is H or a lower alkyl; R5 is H, a (substituted) lower alkyl or an (substituted) acyl; R6 and R7 each is hydroxyl group, and alkoxy or an (substituted) amino] {e.g. diethyl [(E)-3-ethyl-1-hydroxyimino-4-nitro-2-pentenyl]phosphonate}, has strong vasodilator actions and is useful as a therapeutic agent for angina pectoris. The compound is obtained by treating diethyl [1,3- butadienyl]phosphonate expressed by formula II (Et is ethyl) with sodium nitrite.

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